[EN] SUSTITUTED ( HETEROARYLMETHYL ) THIOHYDANTOINS AS ANTICANCER DRUGS<br/>[FR] THIOHYDANTOÏNES (HÉTÉROARYLMÉTHYL) SUBSTITUÉES UTILISÉES COMME MÉDICAMENTS ANTICANCÉREUX
申请人:BAYER SCHERING PHARMA AG
公开号:WO2011029537A1
公开(公告)日:2011-03-17
The invention relates to substituted (heteroarylmethyl) thiohydantoin compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, and their use for the preparation of medicaments for the treatment and/or prophylaxis of disorders, in particular of prostate cancer.
Piperazine derivatives that destabilize androgen receptors
申请人:Schering AG
公开号:US20040009969A1
公开(公告)日:2004-01-15
This invention relates to new piperazine derivatives of general formula I,
1
in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description.
The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostate cancer.
Complex-Induced Proximity Effects in Directed Lithiations: Analysis of Intra- and Intermolecular Kinetic Isotope Effects in Directed Aryl and Benzylic Lithiations
作者:David R. Anderson、Neil C. Faibish、Peter Beak
DOI:10.1021/ja991043m
日期:1999.8.1
mechanism of proton transfers in directedlithiations has been investigated by measuring the intra- and intermolecular kinetic isotope effects for the benzyliclithiation of N-benzyl-N,N‘-dimethyl urea (6) and the ortho lithiations of the tertiary amide N,N-diisopropylbenzamide (7) and the secondary amide N-isopropylbenzamide (8) by sec-BuLi/TMEDA in THF. For the lithiation of 6, a large primary kinetic
[EN] BICYCLIC DERIVATIVES FOR USE IN THE TREATMENT OF ANDROGEN RECEPTOR ASSOCIATED CONDITIONS<br/>[FR] DÉRIVÉS BICYCLIQUES DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT D'AFFECTIONS ASSOCIÉES AU RÉCEPTEUR DES ANDROGÈNES
申请人:ASTRAZENECA AB
公开号:WO2009081197A1
公开(公告)日:2009-07-02
The invention concerns bicyclic compounds of Formula (I), wherein the integers X1, X2, X3, Ring A, R4, R5 and m are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of androgen-receptor associated conditions.
[DE] ANTIANDROGENE PYRROLIDINE MIT TUMORHEMMENDER WIRKSAMKEIT<br/>[EN] ANTITUMORAL ANTIADROGENIC PYRROLIDINES<br/>[FR] PYRROLIDINES ANTIANDROGENES A ACTION ANTITUMORALE
申请人:SCHERING AG
公开号:WO2004099188A1
公开(公告)日:2004-11-18
Die vorliegende Erfindung betrifft antiandrogene N-[w-[3-[4-Cyan-3-(trifluormethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituierte Pyrrolidine der allgemeinen Formel (I), mit einem stark ausgeprägten antiproliferativen Wirkungsprofil; Verfahren zur Herstellung der Verbindungen der allgemeinen Formel (I), pharmazeutische Präparate, und die Verwendung zur Herstellung von Arzneimitteln.